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    • 3. 发明授权
    • Substituted 1-(alkoxy-iminoalkyl) imidazole derivatives and their use in
treating disease related to an enhancement of thromboxane-A.sub.2
syntheis
    • 取代的1-(烷氧基 - 亚氨基烷基)咪唑衍生物及其在治疗与凝血恶烷-A2合成增强有关的疾病中的用途
    • US5280033A
    • 1994-01-18
    • US768568
    • 1991-10-25
    • Paolo CozziMarla MenichincheriArsenia RossiCorrado FertiPatricia Salvati
    • Paolo CozziMarla MenichincheriArsenia RossiCorrado FertiPatricia Salvati
    • A61K31/415A61P3/06A61P13/02A61P15/00A61P43/00C07D233/61C07D521/00C07F7/08A61K31/44C07D409/06
    • C07D231/12C07D233/56C07D249/08C07F7/0812
    • 1-(Alkoxy-iminoalkyl)imidazole derivatives of formula ##STR1## wherein R is hydrogen or C.sub.1 -C.sub.4 alkyl; A is C.sub.1 -C.sub.4 alkylene optionally substituted by phenyl optionally substituted by halogen or trifluoromethyl; R is (a) hydrogen or a C.sub.1 -C.sub.10 hydrocarbon radical; (b) an aryl or aryl-C.sub.1 -C.sub.4 alkyl group wherein the said aryl is optionally substituted either by halogen, trihalo-methyl, C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.3 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio or C.sub.1 -C.sub.4 alkylsulfonyl or by C.sub.5 -C.sub.8 alkyl, C.sub.4 -C.sub.8 alkenyl, C.sub.5 -C.sub.8 alkoxy, C.sub.5 -C.sub.8 alkylthio or phenyl optionally substituted by halogen, trihalomethyl or C.sub.1 -C.sub.4 alkyl; or (c) a C.sub.5 -C.sub.8 cycloalkyl or C.sub.5 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.4 alkyl group, wherein the said cycloalkyl is optionally substituted by C.sub.1 -C.sub.4 alkyl; T is a C.sub.1 -C.sub.6 hydrocarbon chain or phenylene; X is a bond, --O--CH.sub.2 --, --C(R' R")--, Si(R' R")--, vinylene or isopropenylene, each R' and R" being hydrogen, fluorine or C.sub.1 -C.sub.4 alkyl; and R.sub.2 is --OR.sub.3 or --N(R.sub.3 R.sub.4), each R.sub.3 and R.sub.4 being hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl or benzyl; and the pharmaceutically acceptable salts thereof; are useful in the treatment of a disease state related to enhancement of thromboxane A.sub.2 (TxA.sub.2) synthesis.
    • 式(I)的1-(烷氧基亚氨基烷基)咪唑衍生物,其中R是氢或C 1 -C 4烷基; A是任选被任选被卤素或三氟甲基取代的苯基取代的C 1 -C 4亚烷基; R是(a)氢或C 1 -C 10烃基; (b)芳基或芳基-C 1 -C 4烷基,其中所述芳基任选被卤素,三卤代甲基,C 1 -C 4烷基,C 2 -C 3烯基,C 2 -C 6炔基,C 1 -C 4烷氧基, C 1 -C 4烷基磺酰基或C 5 -C 8烷基,C 4 -C 8烯基,C 5 -C 8烷氧基,C 5 -C 8烷硫基或任选被卤素,三卤代甲基或C 1 -C 4烷基取代的苯基; 或(c)C 5 -C 8环烷基或C 5 -C 8环烷基-C 1 -C 4烷基,其中所述环烷基任选被C 1 -C 4烷基取代; T是C1-C6烃链或亚苯基; X是键,-O-CH 2 - , - C(R'R“) - ,Si(R'R”) - 亚乙烯基或异亚丙基,每个R'和R“是氢,氟或C1- C4烷基; 并且R 2是-OR 3或-N(R 3 R 4),每个R 3和R 4是氢,C 1 -C 6烷基,苯基或苄基; 及其药学上可接受的盐; 可用于治疗与凝血恶烷A2(TxA2)合成增强相关的疾病状态。
    • 9. 发明授权
    • Alpha-aminoamide derivatives useful in the treatment of cognitive disorders
    • 可用于治疗认知障碍的α-氨基酰胺衍生物
    • US08741957B2
    • 2014-06-03
    • US12304455
    • 2007-06-13
    • Patricia SalvatiStefano RossettiLuca Benatti
    • Patricia SalvatiStefano RossettiLuca Benatti
    • A61K31/165A61K31/404A61K31/085A61K31/135A61K31/341A61K31/402
    • A61K31/404A61K31/085A61K31/135A61K31/165A61K31/341A61K31/402
    • The present invention is in the field of pharmacotherapy of cognitive deficits in learning and memory by administering an α-aminoamide, particularly safinamide. Examples of disturbances in cognition that can be treated with compounds of the invention are the ones associated with disorders such as autism, dyslexia, attention deficit hyperactivity disorder, schizophrenia, obsessive compulsive disorders, psychosis, bipolar disorders, depression, Tourette's syndrome, Mild Cognitive Impairment (MCI) and disorders of learning in children, adolescents and adults, Age Associated Memory Impairment, Age Associated Cognitive Decline, Alzheimer's Disease, Parkinson's Disease, Down's Syndrome, traumatic brain injury Huntington's Disease, Progressive Supranuclear Palsy (PSP), HIV, stroke, vascular diseases, Pick's or Creutzfeldt-Jacob diseases, multiple sclerosis (MS), other white matter disorders and drug-induced cognitive worsening.
    • 本发明通过给予α-氨基酰胺,特别是safinamide,在学习和记忆中的认知缺陷的药物治疗领域。 可以用本发明化合物治疗的认知障碍的例子是与自闭症,阅读困难,注意缺陷多动障碍,精神分裂症,强迫症,精神病,双相情感障碍,抑郁症,Tourette综合征,轻度认知障碍 (MCI)和儿童,青少年和成年人学习障碍,年龄相关记忆障碍,年龄相关认知衰退,阿尔茨海默病,帕金森病,唐氏综合征,创伤性脑损伤亨廷顿病,进行性核核麻痹(PSP),艾滋病毒,中风, 血管疾病,Pick's或Creutzfeldt-Jacob疾病,多发性硬化症(MS),其他白质病症和药物诱导的认知恶化。